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Investigation of Solubility Enhancement Approaches of Ticagrelor
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ABSTRACT

                   Ticagrelor is an orally administered antiplatelet medicine, direct-acting P2Y12-receptor antagonist. Ticagrelor binds reversibly and noncompetitively to the P2Y12 receptor at a site distinct from that of the endogenous agonist adenosine diphosphate (ADP). Inhibition of platelet aggregation stimulated by ADP is a commonly used pharmacodynamic parameter for P2Y12-receptor antagonists.

                  Ticagrelor is a crystalline powder with an aqueous solubility of approximately 10?g/mL at room temperature. Ticagrelor exhibits no pKa value within the physiological range. Ticagrelor does not exhibit pH-dependent solubility and is defined as ‘low solubility low permeability’ under the Biopharmaceutics Classification System (Class IV). The mean absolute bioavailability of ticagrelor in healthy volunteers is 36 %

                   Nanoparticles preparation and complexation is one of the recently used approaches to enhance the solubility of drugs. The aim of the present work was to improve the solubility and dissolution of ticagrelor by preparing nanoparticles and cyclodextrin inclusion complex of ticagrelor and then incorporated in to tablet dosage form. Fifteen formulas of nanoparticles were prepared by antisolvent precipitation method (solvent displacement method) utilizing one of the three polymers (PVP, Poloxamer, and HPMC) at three different drugs: polymer and solvent: anti-solvent ratios and nine formulas of cyclodextrin inclusion complex with HP?CD  by three preparation methods, physical trituration, kneading and solvent evaporation, which increase the solubility and dissolution rate of ticagrelor via formation of inclusion complex with HP?CD.

              The prepared formulas were characterized regarding the saturated solubility, polydispersity index, particle size by nano laser particle size analyzer, % yield, entrapment efficiency, and flowability, FTIR, DSC, and SEM. The selected formulas were prepared as tablets.

             The prepared tablets were evaluated for drug content, weight variation, hardness, and friability. In vitro dissolution data of the prepared tablets were analyzed using similarity factor (f2) and dissolution efficiency (DE).  

           Among all the prepared nanoparticles formulas, formula (F12) which contain HPMC as a polymer at polymer: drug ratio of (1:1) and solvent: antisolvent ratio of (1:1) was considered as the optimum formula which shows good evaluation parameters in addition to the increment in the solubility to about 9 times than that of the pure drug. The nanoparticle of the selected formula (F12) incorporated tablets showed an acceptable tablet properties in addition to a considerable increase in the dissolution efficiency to (DE=92 % and 88 % in PH 1.2 and PH 6.8 respectively) in comparison to that of the marketed tablet (DE=89% and 85% in PH 1.2 and PH 6.8 respectively).  Moreover, the analysis by DSC and SEM of the nanoparticles of the selected formula (F12) indicate a reduction in the crystallinity and amorphization of the drug. It can be concluded that the selected formula is a promising formula for the preparation of ticagrelor nanoparticles the incorporation in a tablet dosage form.

          Regarding ticagrelor inclusion complex with HP?CD Solvent evaporation method was the most effective method regarding ticagrelor solubilization and optimum formula of inclusion complex (F23) show increment in saturated solubility about ten times that of pure drug.

          The ticagrelor inclusion complex of the selected formula (F23) incorporated tablets showed an acceptable tablet properties in addition to a considerable increase in the dissolution efficiency to (DE=92 % and 90 % in PH 1.2 and PH 6.8 respectively) in comparison to that of the marketed tablet (DE=89% and 85% in PH 1.2 and PH 6.8 respectively).  

 

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Publication Date
Wed Jun 07 2023
Journal Name
Journal Of Educational And Psychological Researches
The Impact of the Sowt Strategy on the Development of Systemic Intelligence among Students of the Ibn Rushd College of Education for the Humanities
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The aim of the current research is to identify the impact of the SWOT strategy on developing systemic intelligence among students of the Ibn Rushd College of Education for Human Sciences University of Baghdad / College of Education Ibn Rushd for Human Sciences. The current research community consists of (8590) male and female students, divided into (7) departments. The current research relied on one of the partial control designs, which is the design of non-random groups: experimental group and a control group with a pre and post-test. As for the research tool, It was represented by Tourmanin’s Systemic Intelligence Scale (2012) of (50) items that measure the eight components of systemic intelligence. The results of the Mann Whitney te

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Publication Date
Tue Jun 30 2020
Journal Name
Journal Of Economics And Administrative Sciences
(Quality and originality in scientific research from the point of view of the participants in the course (qualification of scholars of Bayt al-Hikma)
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Research aims (Quality and originality in scientific research from the point of view of the participants in the course (qualification of scholars of Bayt al-Hikma) To find out how satisfied the participants about the training course held by the house of wisdom (research community), To develop and maximize the capacity of researchers in the field of writing scientific research, As well as establishing frameworks and concepts and standards related to quality and authenticity scientific research, The role played by this kind of research in the service of the movement of the human journey towards progress and prosperity.

On this basis was the research community, their number was (23) common t

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Publication Date
Tue Jun 30 2020
Journal Name
Iraqi Journal Of Market Research And Consumer Protection
DETECTION OF HEAVY METALS POLLUTION INTYPES OF MILK SAMPLES IN BAGHDAD MARKETS: DETECTION OF HEAVY METALS POLLUTION INTYPES OF MILK SAMPLES IN BAGHDAD MARKETS
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The levels of lead (pb), copper (cu), cobalt (co) and cadmium (cd) were determined in different kinds of milk and the health risks were evaluated. The mean levels were 0.73±0.21, 0.06±0.01, 0.12±0.01 and 0.14±0.01 ppm for these metals respectively. The levels of pb and cu were found to be insignificant differences (p<0.05), whereas the levels of co and cd, were no significant differences (p>0.05). The dry and liquid kinds of milk were different significantly (p<0.05), whereas the original, was no significant differences (p>0.05). The values for all metals were more than one. The metals pb and cd were detected at highest concentrations in most dry and liquid milk samples.

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Publication Date
Thu May 14 2020
Journal Name
Journal Of Planner And Development
The Impact of the Method of Dealing with the Product of Wars in the Continuity of the Crisis Wars. Beirut city as an Example
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This research investigates the subject of the impact of wars (as a manifestation of crisis) on architecture, and the extent of continuing wars physical and moral results of wars, even after the end of the cause of the crisis. The impact of different rebuilding which exposed to the effects of the war seems different in crisis regions.

The problem of research is about the uncertainty of the impact of the way chooses for reconstructing the buildings after wars in the continuity of the crisis of war. The goals of this research are to clarify the influence of methods of reconstruction of buildings in a city chosen which is Beirut, on the continuation of the war crisis with the argument of demolishing and rebuilding newly or keeping tr

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Publication Date
Mon Mar 25 2019
Journal Name
Al-academy
The Aesthetic Discourse of the Pop Artists and its Representations in the Output of Students of the Department of Art Education: هند عبدالله عبد
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The emergence of artistic movements in Western countries was after the period of modernity. They have introduced a great dialectical problem at the level of thought and discourse, which necessitated a change in the course of the aesthetic discourse into new visions. Thus, the present research aims to identify the aesthetic discourse of pop artists' Art and its representations in the outputs of the students of the Department of Art Education. The theoretical framework included two sections: the first one, what is the aesthetic discourse and the second is the educational bases of the students' outputs. The procedures of the current research included the analytical descriptive approach. The research sample consisted of (4) outputs chosen ac

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Publication Date
Sun Dec 01 2013
Journal Name
Journal Of Economics And Administrative Sciences
The impact of re-engineering to achieve effective performance level of Ministry of electricity operations/an applied study of process reengineering clean solar cells
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 The study is dealing with an application reengineering process clean solar cells in the Ministry of electricity,  as aimed at the possibility of the applicability and impact of re-engineering to achieve the level of performance of the Ministry's operations, with the application of the cleaning process  solar cells, developed, improved and found a correlation, statistically significant effect between variable re-engineering and performance as well as the application of process reengineering clean solar cells:1- Before the re-engineering process the total time for cleaning up and solar cell 20 minutes and number of columns performed per day 24 columns and total  columns750 which were completed per month that re

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Publication Date
Wed Jun 28 2023
Journal Name
Iraqi Journal Of Market Research And Consumer Protection
PREPARATION OF A COMBINATION OF NANO- MEDICINAL PLANTS AS ANTIOXIDANTS AND MICROORGANISMS: PREPARATION OF A COMBINATION OF NANO- MEDICINAL PLANTS AS ANTIOXIDANTS AND MICROORGANISMS
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ABSTRACT

            The controversy is currently revolving around industrial additives, including antioxidants, their negative effects on consumer health and the emergence of various and various diseases, which led scientists and researchers to intensify most studies on natural antioxidants and their synthesis from medicinal plants mentioned in ancient medicine and in divine books as potential antioxidants of increasing importance. Therefore, this study was designed to synthesize silver nitrate particles from plant leaf extracts (Figs, Olives, and Moringa) and study their effect on bacterial inhibition of each of the undesirable Coliform bacteria (E-Coli,

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Publication Date
Sun Jun 30 2019
Journal Name
Journal Of The College Of Education For Women
The Degree of Practicing of the Sixth Primary Social Studies’ Teachers in Iraq for the Principles of Active Learning from their Point of view
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This study aimed to explore The Degree of Practicing of the Sixth Primary Social Studies’ Teachers in Iraq for the Principles of Active Learning from their Point of view

The study society consisted of 230 male and femalesocial studiesteachers’ subjects for the sixth primary grade in Al-Anbar General Directorate of Education. 160 of them were selected to represent the sample of the study with a percent of (70%) from the original society. To achieve the aims of the study, the researchers prepared a questionnaire consisting of (43) items which represented the active learning principles. The validity and stability of the tool were verified. The researchers used the descriptive approach to suit the objectives of this study. &

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Publication Date
Sat Jan 31 2026
Journal Name
Journal Of Baghdad College Of Dentistry
The effect of orthodontic relapse on the proliferation of fibroblast and epithelial rests of Malassez in periodontal ligament of rat molars (A histopathological study)
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Background: Relapse of previously moved teeth, is major clinical problem in orthodontics with respect to the goals of successful treatment. This study investigated the effect of orthodontic relapse on the proliferation of fibroblast and epithelial rests of Malassez cells in periodontal ligament of rat molars. Materials and Methods: Sixteen ten-week- old male Wister rats were randomly divided into four groups composed of four animals each: Group I received no orthodontic force (control). In both Group II and Group III, uniform standardized expansive springs were used for moving the maxillary first molars buccally for periods of one and three weeks respectively. The spring initially generated an average expansive force of 20 g on each side.

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Publication Date
Mon Feb 28 2022
Journal Name
Journal Of Educational And Psychological Researches
The Impact of the Strategy of Cooperative Integration of Fragmented Information in the Acquisition of Physical Concepts and Science Processes among Fourth Scientific Students
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The current research aims to reveal the impact of the strategy of cooperative integration of fragmented information in the acquisition of physical concepts and science processes among fourth scientific students through the null hypotheses:

1- There is no statistically significant difference at the level of significance (0.05) between the average grades of female students of the experimental group studying physics according to the strategy of cooperative integration of fragmented information and those who follow the traditional method in the test of acquiring physical concepts.

2-There is no statistically significant difference at the level of indication (0.05) between the average grades of female students of the experimen

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